Synthesis and Fungicidal Activities of Nucleoside Compounds Containing Substituted Benzoyl Thiourea

doi:10.6023/cjoc1110111

Chin. J. Org. Chem. ›› 2012, Vol. 32 ›› Issue (05): 915-921.DOI: 10.6023/cjoc1110111 Previous Articles Next Articles

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含取代苯甲酰基硫脲的核苷类化合物的合成及杀菌活性研究

苗宏健^a, 张继伟^a, 袁会珠^b, 李映^a, 徐焱^a, 李慧^a, 杨新玲^a, 凌云^a

a 中国农业大学理学院应用化学系农业部农药化学及应用重点开放实验室北京 100193;
b 中国农业科学院植物保护研究所北京 100193

收稿日期:2011-10-11 修回日期:2011-11-26 发布日期:2012-01-10
通讯作者: 凌云 E-mail:lyun@cau.edu.cn
基金资助:
国家自然科学基金(No. 21072222)、国家973 计划(No. 2010CB126104)和‘十二五’科技支撑计划(No. 2011BAE06B05-5)资助项目.

Synthesis and Fungicidal Activities of Nucleoside Compounds Containing Substituted Benzoyl Thiourea

Miao Hongjian^a, Zhang Jiwei^a, Yuan Huizhu^b, Li Ying^a, Xu Yan^a, Li Hui^a, Yang Xinling^a, Ling Yun^a

a Key Laboratory of Pesticide Chemistry and Application, Ministry of Agriculture, Department of Applied Chemistry,College of Science, China Agricultural University, Beijing 100193;
b Institute of Plant Protection, Chinese Academy of Agricultural Sciences, Beijing 100193

Received:2011-10-11 Revised:2011-11-26 Published:2012-01-10
Supported by:
Project supported by the National Natural Science Foundation of China (No. 21072222), the National Basic Research Program of China (973 Program) (No. 2010CB126104), and the National “Twelfth Five-Year” Plan for Science & Technology Support (No. 2011BAE06B05-5).

To find new fungicidal lead compounds, based on the catalytic mechanism of chitin synthase, a series of novel nucleoside compounds containing thiourea were designed via the method of linking active sub-structures, in which the thiourea with high fungicidal activity was combined to the uridine part of polyoxins and nikkomycins. The target compounds were synthesized from uridine in 5 steps. Their structures were confirmed by IR, ¹H NMR spectra and elemental analysis. The preliminary bioassay results indicated that some compounds showed obvious inhibition effects against Phomopsisasparagi bubak, especially, and the fungicidal activity of 6m (97.2%) at 50 μg/mL is similar to that (100%) of polyoxin B.

Key words: chitin, polyoxins, uridine, thiourea, fungicidal activity

Cite this article

Miao Hongjian, Zhang Jiwei, Yuan Huizhu, Li Ying, Xu Yan, Li Hui, Yang Xinling, Ling Yun. Synthesis and Fungicidal Activities of Nucleoside Compounds Containing Substituted Benzoyl Thiourea[J]. Chin. J. Org. Chem., 2012, 32(05): 915-921.

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含取代苯甲酰基硫脲的核苷类化合物的合成及杀菌活性研究

Synthesis and Fungicidal Activities of Nucleoside Compounds Containing Substituted Benzoyl Thiourea

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